发明名称 TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS WITH SELECTIVE ESTROGEN RECEPTOR MODULATORS
摘要 1. A method of treating, in a patient in need of such treatment, a central nervous system disorder selected from depression, mood swings, and Alzheimer's disease comprising administering a therapeutically effective amount of a compound having the structure or a pharmaceutically acceptable salt or pro-drug thereof, wherein R<1> and R<2> are independently selected from the group consisting of hydroxy and alkoxy of one to four carbon atoms; and R<3> and R<4> are independently selected from methyl or ethyl, or R<3> and R<4>, taken together with the nitrogen atom to which they are attached, form a pyrrolidino, methylpyrrolidino, dimethylpyrrolidino, piperidino, morpholino, or hexamethyleneimino ring. 2. The method of Claim 1 wherein said method comprises treating, in a patient in need of such treatment, depression or mood swings. 3. The method of Claim 1 wherein said method comprises treating, in a patient in need of such treatment, Alzheimer' s disease. 4. The method of Claim 1 wherein R<1> and R<2> are both hydroxy. 5. The method of Claim 2 wherein R<1> and R<2> are both hydroxy. 6. The method of Claim 3 wherein R<1> and R<2> are both hydroxy. 7. The method of Claim 1 wherein R<1> is hydroxy and R<2> is alkoxy of one to four carbon atoms. 8. The method of Claim 2 wherein R<1> is hydroxy and R<2> is alkoxy of one to four carbon atoms. 9. The method of Claim 3 wherein R<1> is hydroxy and R<2> is alkoxy of one to four carbon atoms. 10. The method of Claim 1 wherein R<3> and R<4> combine with the nitrogen atom to which they are attached to form a piperidino ring. 11. The method of Claim 2 wherein R<3> and R<4> combine with the nitrogen atom to which they are attached to form a piperidino ring. 12. The method of Claim 3 wherein R<3> and R<4> combine with the nitrogen atom to which they are attached to form a piperidino ring. 13. A method of treating, in a patient in need of such treatment, depression or mood swings comprising administering a therapeutically effective amount of a compound having the structure or a pharmaceutically acceptable salt or pro-drug thereof, wherein R<2> is hydroxy or methoxy. 14. The method of Claim 13 wherein said compound is 6-hydroxy-2-(4-methoxyphenyl)-3-[4-(2-piperidinoethoxy)-phenoxy]benzo[b]thiophene or a pharmaceutically acceptable salt thereof. 15. The method of Claim 13 wherein said compound is 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)-phenoxy]benzo[b]thiophene or a pharmaceutically acceptable salt thereof. 16. A method of treating, in a patient in need of such treatment, Alzheimer's disease comprising administering a therapeutically effective amount of a compound having the structure or a pharmaceutically acceptable salt or pro-drug thereof, wherein R<2> is hydroxy or methoxy. 17. The method of Claim 16 wherein said compound is 6-hydroxy-2-(4-methoxyphenyl)-3-[4-(2-piperidinoethoxy)-phenoxy]benzo[b]thiophene or a pharmaceutically acceptable salt thereof. 18. The method of Claim 16 wherein said compound is 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)-phenoxy]benzo[b]thiophene or a pharmaceutically acceptable salt thereof. 19. The method of Claim 13 wherein said salt is the hydrochloride salt. 20. The method of Claim 16 wherein said salt is the hydrochloride salt.
申请公布号 EA002360(B1) 申请公布日期 2002.04.25
申请号 EA19990000913 申请日期 1998.04.07
申请人 ELI LILLY AND COMPANY 发明人 BALES, KELLY, RENEE;BRYANT, HENRY, UHLMAN;PAUL, STEVEN, MARC;KNADLER, MARY, PATRICIA
分类号 C07D333/64;A61K31/381;A61K31/4025;A61K31/4535;A61K31/5377;A61K31/55;A61P25/24;A61P25/28 主分类号 C07D333/64
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